Preparation of triazolobenzodiazepine derivatives as Vasopressin V1a antagonists

…, J Newman, C Pasquinet, TM Peakman, T Ryckmans…

Index: Beal, David M.; Bryans, Justin S.; Johnson, Patrick S.; Newman, Julie; Pasquinet, Christelle; Peakman, Torren M.; Ryckmans, Thomas; Underwood, Toby J.; Wheeler, Simon Tetrahedron Letters, 2011 , vol. 52, # 45 p. 5913 - 5917

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Abstract

The arginine Vasopressin V1a receptor is expressed mainly in the liver, vascular smooth muscle cells and the brain. In vascular smooth muscle cells the V1a receptor regulates vasoconstriction and contractility. V1a receptor antagonists have been progressed to the clinic for a range of indications 1 including Raynauds syndrome and dysmenorrhoea. In this Letter we describe the synthesis of a number of fused tricyclic compounds as potential Vasopressin V1a antagonists (Fig. ...

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